Flavonoid-alkylphospholipid conjugates elicit dual inhibition of cancer cell growth and lipid accumulation

Chem Commun (Camb). 2019 Aug 7;55(61):8919-8922. doi: 10.1039/c9cc04084f. Epub 2019 Jul 4.

Abstract

Cancer development is often associated with lipid metabolic reprogramming, including aberrant lipid accumulation. We create novel paradigms endowed with dual functions of anticancer activity and inhibition of lipid accumulation by conjugating the natural product quercetin and synthetic alkylphospholipid drugs, and harnessing the biomedical effects of both. These conjugates offer fresh perspectives in the search for anticancer candidates.

MeSH terms

  • Anti-Obesity Agents / chemical synthesis
  • Anti-Obesity Agents / pharmacology*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Humans
  • Lipid Droplets / metabolism
  • Liver X Receptors / metabolism
  • PPAR gamma / metabolism
  • Phospholipid Ethers / chemical synthesis
  • Phospholipid Ethers / pharmacology*
  • Phosphorylcholine / analogs & derivatives*
  • Phosphorylcholine / chemical synthesis
  • Phosphorylcholine / pharmacology
  • Poly(ADP-ribose) Polymerases / metabolism
  • Proto-Oncogene Proteins c-bcl-2 / metabolism
  • Quercetin / analogs & derivatives*
  • Quercetin / chemical synthesis
  • Quercetin / pharmacology*
  • Signal Transduction / drug effects

Substances

  • Anti-Obesity Agents
  • Antineoplastic Agents
  • BCL2 protein, human
  • Liver X Receptors
  • PPAR gamma
  • Phospholipid Ethers
  • Proto-Oncogene Proteins c-bcl-2
  • Phosphorylcholine
  • edelfosine
  • miltefosine
  • Quercetin
  • Poly(ADP-ribose) Polymerases